生物活性
DIDS sodium salt (MDL101114ZA) is a dual ABCA1 and VDAC1 inhibitor. DIDS sodium salt is also an anion transport inhibitor, which inhibits the ClC-Ka chloride channel and the bacterial ClC-ec1Cl-/H+ exchanger with IC50s of 100 μM and ~300 μM, respectively. DIDS reduced the amplitude of spontaneous transient inward currents (STICs) in a concentration-dependent manner with IC50 value of 2.1 x 10-4M for STICs. Moreover, DIDS was investigated for its action on contraction of cerebral artery smooth muscle cells. DIDS showed a vasodilator effect on pressure-constricted arteries with IC50 of 69 ± 14 μM.
化学数据
分子量 | 498.48 |
分子式 | C16H8N2Na2O6S4 |
CAS号 | 67483-13-0 |
纯度 | >90% |
溶解性(25°C) | DMSO ≥ 25 mg/mL |
储存和运输条件 | -20°C, dry, sealed 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.0061 mL | 10.0305 mL | 20.061 mL |
5 mM | 0.4012 mL | 2.0061 mL | 4.0122 mL |
10 mM | 0.2006 mL | 1.003 mL | 2.0061 mL |